| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Epi-galantamine primarily targets acetylcholinesterase (AChE), the enzyme responsible for the breakdown of the neurotransmitter acetylcholine. By inhibiting AChE with an EC50 of 45.7 μM, it increases acetylcholine levels in the synaptic cleft, enhancing cholinergic transmission. As a diastereomer of galantamine, it shares a similar mechanism of action but with different potency. Galantamine is used clinically for Alzheimer's disease, and epi-galantamine is studied as an impurity and reference standard.
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|---|---|
| ln Vitro |
In vitro, epi-galantamine inhibits acetylcholinesterase (AChE) with an EC50 of 45.7 μM. Its activity is typically evaluated using Ellman's assay, which measures AChE activity by monitoring the hydrolysis of acetylthiocholine. The compound's inhibitory potency is compared to galantamine. However, detailed in vitro data beyond the EC50 value are not extensively reported in the available literature. The compound is primarily used as a reference standard.
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| ln Vivo |
In vivo activity of epi-galantamine has not been extensively characterized in published literature. As a diastereomer of galantamine, it may have similar but less potent effects on cholinergic transmission. However, specific in vivo efficacy data, including dosing regimens and animal models, are not detailed in the available literature. The compound is primarily a research tool and reference standard for galantamine analysis.
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| Enzyme Assay |
Cell-free assays for epi-galantamine involve measuring its inhibitory activity against acetylcholinesterase (AChE). Ellman's assay is commonly used, where AChE hydrolyzes acetylthiocholine to thiocholine, which reacts with DTNB to produce a yellow color. Inhibition is assessed by incubating AChE with varying concentrations of epi-galantamine and measuring residual activity. EC50 values are determined from dose-response curves. The compound's chemical purity and identity are confirmed by HPLC and NMR.
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| Cell Assay |
In vitro cellular assays for epi-galantamine are not typically performed, as the compound is primarily used as a reference standard. If studied, neuronal cell lines would be treated with various concentrations of the compound, and AChE activity in cell lysates would be measured. However, specific assay protocols for this compound are not documented in the available literature. The compound is intended for analytical and research use only.
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| Animal Protocol |
In vivo animal studies for epi-galantamine are not typically conducted, as the compound is primarily used as a reference standard. As a diastereomer of galantamine, it would be expected to have similar but less potent effects in animal models of cholinergic dysfunction. However, specific in vivo data are not available in the published literature. The compound is primarily a research tool for analytical applications.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of epi-galantamine include a molecular weight of 287.35 g/mol and molecular formula C17H21NO3. As an alkaloid, it is expected to have moderate oral bioavailability and blood-brain barrier penetration, similar to galantamine. The compound is typically stored at appropriate conditions as a reference standard. Detailed ADME parameters such as half-life, Cmax, and AUC are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of epi-galantamine has not been extensively characterized in published literature. As a diastereomer of galantamine, it may share some toxicological properties. The compound is intended for research and analytical use only and not for therapeutic applications in humans. Standard safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
According to reports, epigallantanmin is found in Lycoris radiata, daffodils, and other organisms with available data.
Epi-galantamine is a diastereomer of galantamine and an alkaloid from Caucasian snowdrop that inhibits AChE with an EC50 of 45.7 μM. Its molecular formula is C17H21NO3 with a molecular weight of 287.35 g/mol. Epi-galantamine is used as a reference standard and impurity marker for galantamine. It is not for therapeutic use. |
| Molecular Formula |
C₁₇H₂₁NO₃
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|---|---|
| Molecular Weight |
287.35
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| Exact Mass |
287.152
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| CAS # |
1668-85-5
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| PubChem CID |
676392
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.28g/cm3
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| Boiling Point |
439.3ºC at 760 mmHg
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| Melting Point |
183-185ºC
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| Flash Point |
219.5ºC
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| Vapour Pressure |
1.71E-08mmHg at 25°C
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| Index of Refraction |
1.636
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| LogP |
1.788
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
440
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| Defined Atom Stereocenter Count |
3
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| SMILES |
O1C2=C(C([H])=C([H])C3C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])[C@]4(C([H])=C([H])[C@]([H])(C([H])([H])[C@]14[H])O[H])C2=3)OC([H])([H])[H]
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| InChi Key |
ASUTZQLVASHGKV-IFIJOSMWSA-N
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| InChi Code |
InChI=1S/C17H21NO3/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17/h3-6,12,14,19H,7-10H2,1-2H3/t12-,14+,17+/m1/s1
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| Chemical Name |
(1S,12S,14S)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraen-14-ol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4801 mL | 17.4004 mL | 34.8008 mL | |
| 5 mM | 0.6960 mL | 3.4801 mL | 6.9602 mL | |
| 10 mM | 0.3480 mL | 1.7400 mL | 3.4801 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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